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二甲基苯基哌嗪鎓肾上腺素能神经元阻滞作用的特性分析

An analysis of the characteristics of the adrenergic neurone blocking action of dimethylphenylpiperazinium.

作者信息

Jayasundar S, Vohra M M

出版信息

Arch Int Pharmacodyn Ther. 1977 May;227(1):23-9.

PMID:901069
Abstract

An analysis of the characteristics of the adrenergic neurone blocking action of 1,1-dimethyl-4-phenylpiperazinium (DMPP) was undertaken using rat isolated vasa deferentia. DMPP (1 X 10(-6) to 1.5 X 10(-5) g/ml) reduced progressively the contractile response to transmural stimulation (TMS) in a dose-dependent manner without inhibiting the response to exogenous norepinephrine. The DMPP-induced inhibition was not reversed by washing but could be antagonized by dexamphetamine in a concentration which did not by itself affect the response to TMS. Among other sympathomimetic amines tested, it was seen that methamphetamine, ephedrine, phenylpropranolamine and mephentermine were effective in antagonizing DMPP-induce inhibition. High calcium (5 mM) reversed but did not prevent the DMPP-induced inhibition. DMPP reduced preferentially responses to high frequencies of stimulation without affecting those to low.

摘要

利用大鼠离体输精管对1,1 - 二甲基 - 4 - 苯基哌嗪鎓(DMPP)的肾上腺素能神经元阻断作用特性进行了分析。DMPP(1×10⁻⁶至1.5×10⁻⁵克/毫升)以剂量依赖性方式逐渐降低对跨壁刺激(TMS)的收缩反应,而不抑制对外源性去甲肾上腺素的反应。DMPP诱导的抑制作用不能通过冲洗逆转,但可被右旋苯丙胺拮抗,其浓度本身不影响对TMS的反应。在测试的其他拟交感胺中,可见甲基苯丙胺、麻黄碱、苯丙醇胺和美芬丁胺可有效拮抗DMPP诱导的抑制作用。高钙(5毫摩尔)可逆转但不能防止DMPP诱导的抑制作用。DMPP优先降低对高频刺激的反应,而不影响对低频刺激的反应。

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